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BI99179

Names

[ CAS No. ]:
1291779-76-4

[ Name ]:
BI99179

[Synonym ]:
Cyclopentanecarboxamide, N-[4-(2-benzoxazolyl)phenyl]-N-methyl-3-[(1-oxopropyl)amino]-, (1R,3S)-
(1R,3S)-N-[4-(1,3-Benzoxazol-2-yl)phenyl]-N-methyl-3-(propionylamino)cyclopentanecarboxamide

Biological Activity

[Description]:

BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM; demonstrates potent cellular activity (inhibition of 14C-acetate incorporation) with IC50 of 0.6 uM in the mouse N-42 cellular assays, shows no significant LDH release in the cytotoxicity assay at >30 uM; BI-99179 is a tool compound suitable for the in vivo validation of FAS as a therapeutic target.

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Fatty Acid Synthase (FAS)
Research Areas >> Metabolic Disease

[Target]

IC50: 79 nM (FAS)[1]


[In Vitro]

BI 99179 is potent in the mouse hypothalamic N-42 cell with an IC50 of 0.6 μM. BI 99179 shows no significant LDH release in the cytotoxicity assay up to 30 μM[1].

[In Vivo]

BI 99179 has a super pharmacokinetic profile in male Han/Wistar rats (oral application of 4 mg/kg)with half life (t1/2) of 3.0 h[1].

[References]

[1]. Kley JT, et al. Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.Bioorg Med Chem Lett. 2011 Oct 1;21(19):5924-7.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
603.1±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H25N3O3

[ Molecular Weight ]:
391.463

[ Flash Point ]:
318.5±31.5 °C

[ Exact Mass ]:
391.189606

[ LogP ]:
3.12

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.633

Related Compounds